Assay ID | Title | Year | Journal | Article |
AID1559787 | Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 1 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of M |
AID1296529 | Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers. |
AID729274 | Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7
| Structure-activity relationships of peptides incorporating a bioactive reverse-turn heterocycle at the melanocortin receptors: identification of a 5800-fold mouse melanocortin-3 receptor (mMC3R) selective antagonist/partial agonist versus the mouse melano |
AID108614 | Displacement of [125I]NDP-MSH from Melanocortin 1 receptor at 10 uM | 1997 | Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
| Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R. |
AID321769 | Agonist activity at mouse MC3R expressed in HEK293 cells | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
| Backbone cyclic peptidomimetic melanocortin-4 receptor agonist as a novel orally administrated drug lead for treating obesity. |
AID1547514 | Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay | 2020 | ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
| Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy. |
AID109601 | In vitro activation of mouse recombinant Melanocortin-1 receptor. | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
| Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors. 1. Modifications at the His position. |
AID108616 | Inhibitory concentration against human Melanocortin 1 receptor (hMC1R) | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
| Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors. |
AID1479773 | Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors. |
AID109299 | Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
| D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity. |
AID109305 | effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptor | 1997 | Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
| Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R. |
AID108945 | Maximal agonist response at rat melanocortin 3 receptor (MC3R) | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
| De novo design, synthesis, and pharmacology of alpha-melanocyte stimulating hormone analogues derived from somatostatin by a hybrid approach. |
AID1356511 | Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis | | | |
AID1458955 | Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay | 2017 | Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
| Structure-Activity Relationship Studies on a Macrocyclic Agouti-Related Protein (AGRP) Scaffold Reveal Agouti Signaling Protein (ASP) Residue Substitutions Maintain Melanocortin-4 Receptor Antagonist Potency and Result in Inverse Agonist Pharmacology at t |
AID587926 | Agonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Incorporation of a bioactive reverse-turn heterocycle into a peptide template using solid-phase synthesis to probe melanocortin receptor selectivity and ligand conformations by 2D 1H NMR. |
AID252625 | Maximal effect on human melanocortin 5 receptor expressing HEK 293 cells | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues. |
AID1559793 | Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of M |
AID1479776 | Agonist activity at human MC1R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors. |
AID447387 | Agonistic activity against mouse MC4R | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
| Semi-rigid tripeptide agonists of melanocortin receptors. |
AID1725377 | Agonist activity at mouse MC5R by alphascreen cAMP assay | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Peptoid NPhe |
AID246688 | Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4) | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues. |
AID108773 | Percent activation of human melanocortin receptor Melanocortin 3 receptor was determined at 10 uM | 2003 | Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
| Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R. |
AID259549 | Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation. |
AID1559799 | Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of M |
AID1776305 | Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay | 2021 | Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
| Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput "Unbiased" Screening Campaign. |
AID259535 | Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation. |
AID108607 | Evaluated for agonist activity at cloned mammalian human MSH1 receptor | 1995 | Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
| Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors. |
AID109277 | Effective concentration against mouse melanocortin MC4 receptor | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
| Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands. |
AID109111 | Binding affinity for Human Melanocortin 4 receptor expressed in L-cells | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
| D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity. |
AID242174 | Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4) | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues. |
AID109285 | Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132); ND = not determined | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
| Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands. |
AID82379 | In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC1R) | 2003 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
| Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2). |
AID71945 | Relative potency compared to alpha MSH in a frog skin bioassay. | 1997 | Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
| beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity. |
AID1776302 | Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay | 2021 | Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
| Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput "Unbiased" Screening Campaign. |
AID109296 | Effective concentration of peptide at 50% maximal cAMP generation | 2003 | Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
| Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R. |
AID108965 | Effective concentration of peptide at 50% maximal cAMP generation | 2003 | Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
| Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R. |
AID109599 | Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cells | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
| Structure-activity relationships of the melanocortin tetrapeptide Ac-His-D-Phe-Arg-Trp-NH2 at the mouse melanocortin receptors. 4. Modifications at the Trp position. |
AID1725375 | Agonist activity at mouse MC4R by alphascreen cAMP assay | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Peptoid NPhe |
AID259540 | Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation. |
AID109279 | Effective concentration for maximum agonist response towards mouse melanocortin 4 receptor | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
| De novo design, synthesis, and pharmacology of alpha-melanocyte stimulating hormone analogues derived from somatostatin by a hybrid approach. |
AID1476413 | Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay relative to alpha-MSH | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
| Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists. |
AID108636 | Effective concentration against mouse Melanocortin 1 receptor | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
| Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands. |
AID391362 | Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity. |
AID1559796 | Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of M |
AID1559777 | Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of M |
AID107046 | Agonist activity towards mouse Melanocortin-5 receptor (mMC5R) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors: part 2 modifications at the Phe position. |
AID109447 | Maximum agonist response for mouse melanocortin 5 receptor (MC5R) | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
| De novo design, synthesis, and pharmacology of alpha-melanocyte stimulating hormone analogues derived from somatostatin by a hybrid approach. |
AID82380 | In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R) | 2003 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
| Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2). |
AID1725370 | Agonist activity at mouse MC1R by alphascreen cAMP assay | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Peptoid NPhe |
AID71942 | Decrease in frog skin reflectivity (metabotropic activity). | 1997 | Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
| beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity. |
AID33850 | Inhibition of human adenosine deaminase (ADA) | 2004 | Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
| Structure-based design, synthesis, and structure-activity relationship studies of novel non-nucleoside adenosine deaminase inhibitors. |
AID259551 | Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation. |
AID240051 | In vitro agonist potency for Mouse Melanocortin 1 receptor | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
| N-terminal fatty acylated His-dPhe-Arg-Trp-NH(2) tetrapeptides: influence of fatty acid chain length on potency and selectivity at the mouse melanocortin receptors and human melanocytes. |
AID259547 | Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation. |
AID109283 | Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determined | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
| Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands. |
AID1428575 | Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay | 2017 | Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
| A Macrocyclic Agouti-Related Protein/[Nle |
AID102011 | Decrease in lizard skin reflectivity (metabotropic activity). | 1997 | Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
| beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity. |
AID1458956 | Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay | 2017 | Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
| Structure-Activity Relationship Studies on a Macrocyclic Agouti-Related Protein (AGRP) Scaffold Reveal Agouti Signaling Protein (ASP) Residue Substitutions Maintain Melanocortin-4 Receptor Antagonist Potency and Result in Inverse Agonist Pharmacology at t |
AID109446 | Effective concentration against mouse Melanocortin 5 receptor | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
| Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands. |
AID108798 | Binding affinity towards human Melanocortin 3 receptor (hMC3R) | 2003 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
| Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2). |
AID1559790 | Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of M |
AID1559780 | Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of M |
AID1356510 | Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis | | | |
AID252624 | Maximal effect on human melanocortin 4 receptor expressing HEK 293 cells | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues. |
AID1296535 | Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers. |
AID221830 | Functional activity at the mouse melanocortin 1 receptor | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13
| Characterization of melanocortin NDP-MSH agonist peptide fragments at the mouse central and peripheral melanocortin receptors. |
AID321787 | Agonist activity at mouse MC1R expressed in HEK293 cells | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
| Backbone cyclic peptidomimetic melanocortin-4 receptor agonist as a novel orally administrated drug lead for treating obesity. |
AID1479772 | Agonist activity at mouse MC1R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors. |
AID108939 | Effective concentration against mouse Melanocortin 3 receptor | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
| Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands. |
AID107034 | In vitro activation of mouse recombinant Melanocortin-4 receptor. | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
| Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors. 1. Modifications at the His position. |
AID1151527 | Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs). |
AID259546 | Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation. |
AID1356509 | Agonist activity at mouse MC4R expressed in HEK293 cells at 100 uM incubated for 2 hrs by AlphaScreen cAMP assay relative to untreated control | | | |
AID346427 | Displacement of radiolabeled NDPalpha-MSH from human MC4 receptor | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. |
AID391354 | Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity. |
AID259542 | Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation. |
AID109127 | Inhibitory activity against human Melanocortin 4 receptor | 1995 | Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
| Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors. |
AID1476417 | Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
| Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists. |
AID282351 | Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
| Stereochemical studies of the monocyclic agouti-related protein (103-122) Arg-Phe-Phe residues: conversion of a melanocortin-4 receptor antagonist into an agonist and results in the discovery of a potent and selective melanocortin-1 agonist. |
AID107033 | Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cells | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
| Structure-activity relationships of the melanocortin tetrapeptide Ac-His-D-Phe-Arg-Trp-NH2 at the mouse melanocortin receptors. 4. Modifications at the Trp position. |
AID240566 | Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4 | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues. |
AID108968 | Effective concentration required for the biological activity against human Melanocortin 4 receptor | 2003 | Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20
| Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes. |
AID1479774 | Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors. |
AID259543 | Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation. |
AID108795 | Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM | 1997 | Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
| Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R. |
AID1476419 | Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay relative to alpha-MSH | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
| Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists. |
AID242173 | Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4) | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues. |
AID1483077 | Agonist activity at mouse MC4R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa |
AID109614 | Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
| Structure-activity relationships of the melanocortin tetrapeptide Ac-His-D-Phe-Arg-Trp-NH2 at the mouse melanocortin receptors. 4. Modifications at the Trp position. |
AID1685034 | Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay | | | |
AID677159 | Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues. |
AID632881 | Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
| Development of melanoma-targeted polymer micelles by conjugation of a melanocortin 1 receptor (MC1R) specific ligand. |
AID108952 | Percent activation of human melanocortin receptor human Melanocortin 4 receptor was determined at 10 uM | 2003 | Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
| Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R. |
AID109453 | Agonist activity against human melanocortin receptor hMC1R | 2003 | Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
| Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: histidine substitution. |
AID108622 | Binding affinity towards human Melanocortin 1 receptor (hMC1R) | 2003 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
| Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2). |
AID246686 | Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4) | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues. |
AID1296527 | Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers. |
AID447386 | Agonistic activity against mouse MC3R | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
| Semi-rigid tripeptide agonists of melanocortin receptors. |
AID240039 | Effective concentration for mouse Melanocortin-1 receptor | 2005 | Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
| Structure-activity relationships of the unique and potent agouti-related protein (AGRP)-melanocortin chimeric Tyr-c[beta-Asp-His-DPhe-Arg-Trp-Asn-Ala-Phe-Dpr]-Tyr-NH2 peptide template. |
AID108957 | Agonist potency towards human Melanocortin 4 receptor | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17
| Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: arginine substitution. |
AID246687 | Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4) | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues. |
AID259545 | Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation. |
AID108777 | Effective concentration of peptide at 50% maximal cAMP generation | 2003 | Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
| Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R. |
AID1483081 | Agonist activity at mouse MC1R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa |
AID109119 | Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM | 1997 | Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
| Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R. |
AID108937 | Compound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cells | 2003 | Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
| Urea small molecule agonists on mouse melanocortin receptors. |
AID1483084 | Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa |
AID677161 | Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues. |
AID1483091 | Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa |
AID1151525 | Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs). |
AID109107 | effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor | 1997 | Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
| Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R. |
AID677158 | Displacement of [125I]-NAD-alpha-MSH from human recombinant MC1 receptor expressed in BHK570 cells after 90 mins in presence of ovalbumin | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues. |
AID1428576 | Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay | 2017 | Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
| A Macrocyclic Agouti-Related Protein/[Nle |
AID108794 | Inhibitory concentration against human Melanocortin 3 receptor (hMC3R) | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
| Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors. |
AID632884 | Selectivity ratio of Ki for human MC5 receptor expressed in human HEK293 cells to Ki for human MC1 receptor expressed in human HCT116 cells | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
| Development of melanoma-targeted polymer micelles by conjugation of a melanocortin 1 receptor (MC1R) specific ligand. |
AID1356503 | Agonist activity at mouse MC1R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay | | | |
AID677162 | Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues. |
AID1169942 | Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
| 1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity. |
AID1476411 | Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
| Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists. |
AID1771945 | Agonist activity at mouse MC1R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Functional Mixture-Based Positional Scan Identifies a Library of Antagonist Tetrapeptide Sequences (LAtTeS) with Nanomolar Potency for the Melanocortin-4 Receptor and Equipotent with the Endogenous AGRP(86-132) Antagonist. |
AID751880 | Binding affinity to human MC4 receptor by radioligand displacement assay | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds. |
AID1151524 | Agonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs). |
AID391356 | Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity. |
AID259541 | Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation. |
AID1476414 | Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
| Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists. |
AID259534 | Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation. |
AID240052 | In vitro agonist potency for Mouse Melanocortin 3 receptor | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
| N-terminal fatty acylated His-dPhe-Arg-Trp-NH(2) tetrapeptides: influence of fatty acid chain length on potency and selectivity at the mouse melanocortin receptors and human melanocytes. |
AID109602 | Agonist activity to the mouse Melanocortin-1 receptor (mMC1R) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors: part 2 modifications at the Phe position. |
AID109429 | Inhibitory concentration against human Melanocortin 5 receptor (hMC5R) | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
| Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors. |
AID259544 | Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation. |
AID259548 | Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation. |
AID108637 | Maximal agonist response of mouse melanocortin 1 receptor (MC1R) | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
| De novo design, synthesis, and pharmacology of alpha-melanocyte stimulating hormone analogues derived from somatostatin by a hybrid approach. |
AID108604 | Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 1 receptor | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
| Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors. |
AID252623 | Maximal effect on human melanocortin 3 receptor expressing HEK 293 cells | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues. |
AID321771 | Agonist activity at mouse MC5R expressed in HEK293 cells | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
| Backbone cyclic peptidomimetic melanocortin-4 receptor agonist as a novel orally administrated drug lead for treating obesity. |
AID108775 | Maximum accumulation of cAMP level against Melanocortin 3 receptor at 10 uM | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
| D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity. |
AID1479778 | Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors. |
AID240053 | In vitro agonist potency for Mouse Melanocortin 4 receptor | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
| N-terminal fatty acylated His-dPhe-Arg-Trp-NH(2) tetrapeptides: influence of fatty acid chain length on potency and selectivity at the mouse melanocortin receptors and human melanocytes. |
AID109425 | Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM | 1997 | Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
| Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R. |
AID259536 | Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation. |
AID109306 | Binding affinity for Human Melanocortin 5 receptor expressed in L-cells | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
| D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity. |
AID107045 | In vitro activation of mouse recombinant Melanocortin-5 receptor. | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
| Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors. 1. Modifications at the His position. |
AID321768 | Displacement of [125I]NDP-alpha-MSH from MC4R | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
| Backbone cyclic peptidomimetic melanocortin-4 receptor agonist as a novel orally administrated drug lead for treating obesity. |
AID259537 | Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation. |
AID282353 | Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
| Stereochemical studies of the monocyclic agouti-related protein (103-122) Arg-Phe-Phe residues: conversion of a melanocortin-4 receptor antagonist into an agonist and results in the discovery of a potent and selective melanocortin-1 agonist. |
AID1356506 | Inverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay | | | |
AID1638719 | Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Discovery of Polypharmacological Melanocortin-3 and -4 Receptor Probes and Identification of a 100-Fold Selective nM MC3R Agonist versus a μM MC4R Partial Agonist. |
AID1483074 | Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa |
AID109462 | Agonist activity against human melanocortin receptor hMC4R | 2003 | Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
| Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: histidine substitution. |
AID1638723 | Full agonist activity at mouse MC1R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Discovery of Polypharmacological Melanocortin-3 and -4 Receptor Probes and Identification of a 100-Fold Selective nM MC3R Agonist versus a μM MC4R Partial Agonist. |
AID1479777 | Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors. |
AID104102 | Effective concentration was measured against frog skin MCR cells at 10 e-4 10 e-12 M Concentration. | 1997 | Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
| Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R. |
AID240040 | Effective concentration for mouse Melanocortin-3 receptor | 2005 | Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
| Structure-activity relationships of the unique and potent agouti-related protein (AGRP)-melanocortin chimeric Tyr-c[beta-Asp-His-DPhe-Arg-Trp-Asn-Ala-Phe-Dpr]-Tyr-NH2 peptide template. |
AID1476421 | Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay relative to alpha-MSH | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
| Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists. |
AID729277 | Agonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7
| Structure-activity relationships of peptides incorporating a bioactive reverse-turn heterocycle at the melanocortin receptors: identification of a 5800-fold mouse melanocortin-3 receptor (mMC3R) selective antagonist/partial agonist versus the mouse melano |
AID732393 | Cytotoxicity against human HEK293 cells assessed as cell viability at 100 uM to 1 uM upto 48 hrs | | | |
AID108786 | effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor | 1997 | Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
| Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R. |
AID259553 | Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation. |
AID108481 | Agonist potency for human Melanocortin 1 receptor | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17
| Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: arginine substitution. |
AID1685031 | Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay | | | |
AID259552 | Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation. |
AID109617 | Agonist activity to the mouse Melanocortin-3 receptor (mMC3R) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors: part 2 modifications at the Phe position. |
AID102012 | In vitro potency of compound to stimulate melanosome dispersion in lizard skin relative to alpha-MSH | 1982 | Journal of medicinal chemistry, Sep, Volume: 25, Issue:9
| Comparative biological activities of highly potent active-site analogues of alpha-melanotropin. |
AID108781 | Evaluated for agonist activity at cloned Melanocortin 3 receptor | 1995 | Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
| Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors. |
AID221832 | Functional activity at the mouse melanocortin 3 receptor | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13
| Characterization of melanocortin NDP-MSH agonist peptide fragments at the mouse central and peripheral melanocortin receptors. |
AID1458954 | Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay | 2017 | Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
| Structure-Activity Relationship Studies on a Macrocyclic Agouti-Related Protein (AGRP) Scaffold Reveal Agouti Signaling Protein (ASP) Residue Substitutions Maintain Melanocortin-4 Receptor Antagonist Potency and Result in Inverse Agonist Pharmacology at t |
AID1685033 | Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay | | | |
AID752240 | Binding affinity to human MC4 receptor by radioligand displacement assay | 2013 | Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
| Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor. |
AID109298 | Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
| Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors. |
AID71943 | In vitro potency of compound to stimulate melanosome dispersion in frog (Rana pipiens) skin relative to alpha-MSH | 1982 | Journal of medicinal chemistry, Sep, Volume: 25, Issue:9
| Comparative biological activities of highly potent active-site analogues of alpha-melanotropin. |
AID108792 | Inhibition of human Melanocortin 3 receptor | 2003 | Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
| Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R. |
AID108605 | Effective concentration required for the biological activity against human Melanocortin 1 receptor | 2003 | Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20
| Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes. |
AID109291 | Maximum accumulation of cAMP by Melanocortin 5 receptor at 10 uM | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
| D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity. |
AID282350 | Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assay | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
| Stereochemical studies of the monocyclic agouti-related protein (103-122) Arg-Phe-Phe residues: conversion of a melanocortin-4 receptor antagonist into an agonist and results in the discovery of a potent and selective melanocortin-1 agonist. |
AID109444 | Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells | 2003 | Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
| Urea small molecule agonists on mouse melanocortin receptors. |
AID1336329 | Displacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting method | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
| Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
AID282355 | Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
| Stereochemical studies of the monocyclic agouti-related protein (103-122) Arg-Phe-Phe residues: conversion of a melanocortin-4 receptor antagonist into an agonist and results in the discovery of a potent and selective melanocortin-1 agonist. |
AID1296534 | Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers. |
AID1771950 | Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Functional Mixture-Based Positional Scan Identifies a Library of Antagonist Tetrapeptide Sequences (LAtTeS) with Nanomolar Potency for the Melanocortin-4 Receptor and Equipotent with the Endogenous AGRP(86-132) Antagonist. |
AID108969 | Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
| D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity. |
AID1483073 | Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa |
AID102013 | Relative potency compared to alpha MSH in a lizard skin bioassay. | 1997 | Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
| beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity. |
AID677160 | Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues. |
AID108956 | Maximum accumulation of cAMP level by Melanocortin 4 receptor at 10 uM | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
| D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity. |
AID1285634 | Displacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cells | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
| Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents. |
AID1479775 | Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors. |
AID587930 | Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Incorporation of a bioactive reverse-turn heterocycle into a peptide template using solid-phase synthesis to probe melanocortin receptor selectivity and ligand conformations by 2D 1H NMR. |
AID221834 | Functional activity at the mouse melanocortin 4 receptor | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13
| Characterization of melanocortin NDP-MSH agonist peptide fragments at the mouse central and peripheral melanocortin receptors. |
AID1771948 | Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP level incubated for 2 hr by alphaScreen assay | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Functional Mixture-Based Positional Scan Identifies a Library of Antagonist Tetrapeptide Sequences (LAtTeS) with Nanomolar Potency for the Melanocortin-4 Receptor and Equipotent with the Endogenous AGRP(86-132) Antagonist. |
AID240054 | In vitro agonist potency for Mouse Melanocortin 5 receptor | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
| N-terminal fatty acylated His-dPhe-Arg-Trp-NH(2) tetrapeptides: influence of fatty acid chain length on potency and selectivity at the mouse melanocortin receptors and human melanocytes. |
AID587928 | Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Incorporation of a bioactive reverse-turn heterocycle into a peptide template using solid-phase synthesis to probe melanocortin receptor selectivity and ligand conformations by 2D 1H NMR. |
AID108787 | Binding affinity for Human Melanocortin 3 receptor expressed in L-cells | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
| D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity. |
AID447388 | Agonistic activity against mouse MC5R | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
| Semi-rigid tripeptide agonists of melanocortin receptors. |
AID1776311 | Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay | 2021 | Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
| Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput "Unbiased" Screening Campaign. |
AID259538 | Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation. |
AID107044 | Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cells | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
| Structure-activity relationships of the melanocortin tetrapeptide Ac-His-D-Phe-Arg-Trp-NH2 at the mouse melanocortin receptors. 4. Modifications at the Trp position. |
AID108611 | effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 1 receptor | 1997 | Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
| Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R. |
AID1685035 | Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay | | | |
AID108778 | Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
| Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors. |
AID1169944 | Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
| 1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity. |
AID109131 | Inhibitory concentration against human Melanocortin 4 receptor (hMC4R) | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
| Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors. |
AID321770 | Agonist activity at mouse MC4R expressed in HEK293 cells | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
| Backbone cyclic peptidomimetic melanocortin-4 receptor agonist as a novel orally administrated drug lead for treating obesity. |
AID240041 | Effective concentration for mouse Melanocortin-4 receptor | 2005 | Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
| Structure-activity relationships of the unique and potent agouti-related protein (AGRP)-melanocortin chimeric Tyr-c[beta-Asp-His-DPhe-Arg-Trp-Asn-Ala-Phe-Dpr]-Tyr-NH2 peptide template. |
AID1547509 | Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP AlphaScreen assay | 2020 | ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
| Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy. |
AID1705453 | Photo-protective activity in EPP patient assessed as time spent in direct sunlight without pain measured after 6 months (Rvb = 41 hrs) | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | New drug approvals for 2019: Synthesis and clinical applications. |
AID109289 | Percent activation of human melanocortin receptor Melanocortin 5 receptor was determined at 10 uM | 2003 | Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
| Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R. |
AID1725372 | Agonist activity at mouse MC3R by alphascreen cAMP assay | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Peptoid NPhe |
AID34307 | In vitro potency of compound to stimulate adenylate cyclase activity in melanoma cells relative to alpha-MSH | 1982 | Journal of medicinal chemistry, Sep, Volume: 25, Issue:9
| Comparative biological activities of highly potent active-site analogues of alpha-melanotropin. |
AID729276 | Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7
| Structure-activity relationships of peptides incorporating a bioactive reverse-turn heterocycle at the melanocortin receptors: identification of a 5800-fold mouse melanocortin-3 receptor (mMC3R) selective antagonist/partial agonist versus the mouse melano |
AID729275 | Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7
| Structure-activity relationships of peptides incorporating a bioactive reverse-turn heterocycle at the melanocortin receptors: identification of a 5800-fold mouse melanocortin-3 receptor (mMC3R) selective antagonist/partial agonist versus the mouse melano |
AID1547511 | Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay | 2020 | ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
| Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy. |
AID632883 | Selectivity ratio of Ki for human MC4 receptor expressed in human HEK293 cells to Ki for human MC1 receptor expressed in human HCT116 cells | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
| Development of melanoma-targeted polymer micelles by conjugation of a melanocortin 1 receptor (MC1R) specific ligand. |
AID1151529 | Displacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cells | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs). |
AID108790 | Inhibitory activity against Melanocortin 3 receptor | 1995 | Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
| Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors. |
AID447385 | Agonistic activity against mouse MC1R | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
| Semi-rigid tripeptide agonists of melanocortin receptors. |
AID109275 | Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells | 2003 | Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
| Urea small molecule agonists on mouse melanocortin receptors. |
AID240042 | Effective concentration for mouse Melanocortin-5 receptor | 2005 | Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
| Structure-activity relationships of the unique and potent agouti-related protein (AGRP)-melanocortin chimeric Tyr-c[beta-Asp-His-DPhe-Arg-Trp-Asn-Ala-Phe-Dpr]-Tyr-NH2 peptide template. |
AID632880 | Displacement of Eu-NDP-alphaMSH from human MC1 receptor expressed in human HCT116 cells after 1.5 hrs by time-resolved fluorescence analysis | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
| Development of melanoma-targeted polymer micelles by conjugation of a melanocortin 1 receptor (MC1R) specific ligand. |
AID1776308 | Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay | 2021 | Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
| Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput "Unbiased" Screening Campaign. |
AID1169943 | Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
| 1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity. |
AID391365 | Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity. |
AID1638724 | Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Discovery of Polypharmacological Melanocortin-3 and -4 Receptor Probes and Identification of a 100-Fold Selective nM MC3R Agonist versus a μM MC4R Partial Agonist. |
AID1476416 | Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay relative to alpha-MSH | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
| Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists. |
AID259550 | Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation. |
AID1296528 | Displacement of 125I-NDP-MSH from mouse MC1R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers. |
AID1476420 | Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
| Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists. |
AID632882 | Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
| Development of melanoma-targeted polymer micelles by conjugation of a melanocortin 1 receptor (MC1R) specific ligand. |
AID108780 | Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
| D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity. |
AID108970 | Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptor | 1995 | Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
| Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors. |
AID1638718 | Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Discovery of Polypharmacological Melanocortin-3 and -4 Receptor Probes and Identification of a 100-Fold Selective nM MC3R Agonist versus a μM MC4R Partial Agonist. |
AID108967 | Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
| Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors. |
AID1458957 | Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay | 2017 | Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
| Structure-Activity Relationship Studies on a Macrocyclic Agouti-Related Protein (AGRP) Scaffold Reveal Agouti Signaling Protein (ASP) Residue Substitutions Maintain Melanocortin-4 Receptor Antagonist Potency and Result in Inverse Agonist Pharmacology at t |
AID109428 | Inhibition of human melanocortin 5 receptor | 2003 | Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
| Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R. |
AID1559775 | Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of M |
AID1559783 | Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of M |
AID109128 | Inhibition of human melanocortin 4 receptor | 2003 | Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
| Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R. |
AID108779 | Effective concentration required for the biological activity against human Melanocortin 3 receptor | 2003 | Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20
| Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes. |
AID82381 | In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R) | 2003 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
| Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2). |
AID252622 | Maximal effect on human melanocortin 1 receptor expressing HEK 293 cells | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues. |
AID1296537 | Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers. |
AID1356508 | Agonist activity at mouse MC3R expressed in HEK293 cells at 100 uM incubated for 2 hrs by AlphaScreen cAMP assay relative to untreated control | | | |
AID1169945 | Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
| 1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity. |
AID1547516 | Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay | 2020 | ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
| Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy. |
AID1151528 | Displacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cells | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs). |
AID259539 | Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation. |
AID587929 | Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Incorporation of a bioactive reverse-turn heterocycle into a peptide template using solid-phase synthesis to probe melanocortin receptor selectivity and ligand conformations by 2D 1H NMR. |
AID108634 | Agonist activity on mouse melanocortin 1 receptor (mMC1R) stably expressed in HEK cells | 2003 | Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
| Urea small molecule agonists on mouse melanocortin receptors. |
AID1151526 | Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs). |
AID1296536 | Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers. |
AID1428577 | Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay | 2017 | Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
| A Macrocyclic Agouti-Related Protein/[Nle |
AID109615 | In vitro activation of mouse recombinant Melanocortin-3 receptor. | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
| Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors. 1. Modifications at the His position. |
AID107035 | Agonist activity to the mouse Melanocortin-4 receptor (mMC4R) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors: part 2 modifications at the Phe position. |
AID221835 | Functional activity at the mouse melanocortin 5 receptor | 2001 | Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13
| Characterization of melanocortin NDP-MSH agonist peptide fragments at the mouse central and peripheral melanocortin receptors. |
AID1479779 | Agonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors. |
AID1428574 | Agonist activity at mouse MC1R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay | 2017 | Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
| A Macrocyclic Agouti-Related Protein/[Nle |
AID109137 | Binding affinity towards human melanocortin 4 receptor (hMC4R) | 2003 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
| Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2). |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |